Abstract
Proteases constitute one of the primary targets in drug discovery. In the present review, we focus on extracellular proteases (ECPs) because of their differential expression in many pathophysiological processes, including cancer, cardiovascular conditions, and inflammatory, pulmonary, and periodontal diseases. Many new ECP inhibitors are currently under clinical investigation and a significant increase in new therapies based on protease inhibition can be expected in the coming years. In addition to directly blocking the activity of a targeted protease, one can take advantage of differential expression in disease states to selectively deliver therapeutic or imaging agents. Recent studies in targeted drug development for the metalloproteases (matrix metalloproteinases, adamalysins, pappalysins, neprilysin, angiotensin-converting enzyme, metallocarboxypeptidases, and glutamate carboxypeptidase II), serine proteases (elastase, coagulation factors, tissue/urokinase plasminogen activator system, kallikreins, tryptase, dipeptidyl peptidase IV) and cysteine proteases (cathepsin B) are discussed herein.
Keywords: Drug targets, extracellular proteases, metalloproteases, serine proteases, cysteine proteases, protease inhibitors
Current Protein & Peptide Science
Title: Extracellular Proteases as Targets for Drug Development
Volume: 10 Issue: 4
Author(s): Mare Cudic and Gregg B. Fields
Affiliation:
Keywords: Drug targets, extracellular proteases, metalloproteases, serine proteases, cysteine proteases, protease inhibitors
Abstract: Proteases constitute one of the primary targets in drug discovery. In the present review, we focus on extracellular proteases (ECPs) because of their differential expression in many pathophysiological processes, including cancer, cardiovascular conditions, and inflammatory, pulmonary, and periodontal diseases. Many new ECP inhibitors are currently under clinical investigation and a significant increase in new therapies based on protease inhibition can be expected in the coming years. In addition to directly blocking the activity of a targeted protease, one can take advantage of differential expression in disease states to selectively deliver therapeutic or imaging agents. Recent studies in targeted drug development for the metalloproteases (matrix metalloproteinases, adamalysins, pappalysins, neprilysin, angiotensin-converting enzyme, metallocarboxypeptidases, and glutamate carboxypeptidase II), serine proteases (elastase, coagulation factors, tissue/urokinase plasminogen activator system, kallikreins, tryptase, dipeptidyl peptidase IV) and cysteine proteases (cathepsin B) are discussed herein.
Export Options
About this article
Cite this article as:
Cudic Mare and Fields B. Gregg, Extracellular Proteases as Targets for Drug Development, Current Protein & Peptide Science 2009; 10 (4) . https://dx.doi.org/10.2174/138920309788922207
DOI https://dx.doi.org/10.2174/138920309788922207 |
Print ISSN 1389-2037 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5550 |
Call for Papers in Thematic Issues
Advancements in Proteomic and Peptidomic Approaches in Cancer Immunotherapy: Unveiling the Immune Microenvironment
The scope of this thematic issue centers on the integration of proteomic and peptidomic technologies into the field of cancer immunotherapy, with a particular emphasis on exploring the tumor immune microenvironment. This issue aims to gather contributions that illustrate the application of these advanced methodologies in unveiling the complex interplay ...read more
Nutrition and Metabolism in Musculoskeletal Diseases
The musculoskeletal system consists mainly of cartilage, bone, muscles, tendons, connective tissue and ligaments. Balanced metabolism is of vital importance for the homeostasis of the musculoskeletal system. A series of musculoskeletal diseases (for example, sarcopenia, osteoporosis) are resulted from the dysregulated metabolism of the musculoskeletal system. Furthermore, metabolic diseases (such ...read more
Protein Folding, Aggregation and Liquid-Liquid Phase Separation
Protein folding, misfolding and aggregation remain one of the main problems of interdisciplinary science not only because many questions are still open, but also because they are important from the point of view of practical application. Protein aggregation and formation of fibrillar structures, for example, is a hallmark of a ...read more
Related Journals
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Matrix Metalloproteinases as Valid Clinical Target
Current Pharmaceutical Design Proteomics and Epigenetic Mechanisms in Stem Cells
Current Proteomics Wound Dressing Based Collagen Biomaterials Containing Usnic Acid as Quorum Sensing Inhibitor Agent: Synthesis, Characterization and Bioevaluation
Current Organic Chemistry Therapeutic Implications of Superoxide Dismutase And Its Importance in Kinase Drug Discovery
Current Topics in Medicinal Chemistry Plant Polyphenols and Oral Health: Old Phytochemicals for New Fields
Current Medicinal Chemistry Potential Therapeutic Benefits of Dipyridamole in COVID-19 Patients
Current Pharmaceutical Design Application of Molecular Topology to the Search of Novel NSAIDs: Experimental Validation of Activity
Letters in Drug Design & Discovery OIP5-AS1: A Fascinating Long Noncoding RNA in Carcinoma
Current Pharmaceutical Design Antioxidant Response of Osteoblasts to Doxycycline in an Inflammatory Model Induced by C-reactive Protein and Interleukin-6
Infectious Disorders - Drug Targets Matrixmetalloproteinase Inhibitors: Promising Therapeutic Targets Against Cancer
Current Pharmaceutical Design Periodontitis and Periodontal Disease - Innovative Strategies for Reversing the Chronic Infectious and Inflammatory Condition by Natural Products
Current Pharmaceutical Design Biomarkers of Regenerative Responses to Phenytoin in Periosteal Fibroblasts and Modulation by Histamine; Relevance to Inflammatory Repair
Recent Patents on Biomarkers Fast Dissolving Films: A Review
Current Drug Delivery Periodontal Diseases and Rheumatoid Arthritis: A Coincident Model for Therapeutic Intervention?
Current Drug Metabolism Editorial [Hot Topic: Chemical Approaches to Anti-Inflammatory Discovery (Guest Editor: Balbina J. Plotkin)]
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Preparation, Physicochemical Evaluation and Characterization of Mucoadhesive Buccal Gels Impregnated with Benzydamine Hydrochloride for the Effective Treatment of Aphthous Stomatitis: Effect of Different Grades of HPMC Polymer on In vitro and Ex vivo Performance
Drug Delivery Letters Investigation of Methylene Blue Release from Functional Polymeric Systems Using Dielectric Analysis
Current Drug Delivery Opportunities Offered by Chitosan-Based Nanotechnology in Mucosal/ Skin Drug Delivery
Current Topics in Medicinal Chemistry Recent Patents Review in Microencapsulation of Pharmaceuticals Using the Emulsion Solvent Removal Methods
Recent Patents on Drug Delivery & Formulation Immune Response Studies Based on P2X7 Receptors: A Mini-Review
Current Pharmaceutical Design